Biological Activity
p-iodo-clonidine (hydrochloride) is a partial agonist of the alpha 2-adrenergic receptor [1].the adrenergic receptors are g protein-coupled receptors that are targets of the catecholamines, especially norepinephrine and epinephrine. there are two main groups of adrenergic receptors: α receptors and β receptors. α2-adrenergic receptor is a gi coupled receptor, which causes a decrease in neurotransmitter release, as well as a decrease of camp activity resulting in smooth muscle contraction [1].p-iodo-clonidine (hydrochloride) is a partial agonist of the alpha 2-adrenergic receptor. clonidine is an antihypertensive α2-adrenergic receptor agonist. pic had minimal agonist activity in inhibiting adenylate cyclase in platelet membranes through α2-adrenergic receptor, but it increased platelet aggregation induced by adp with ec50 value of 1.5 μm. pic also inhibited epinephrine-induced aggregation with ic50 value of 5.1 μm. pic competed for [3h]bromoxidine binding with ki value of 1.0 nm. pic bound to the alpha 2b-ar in ng-10815 cell membranes with kd value of 0.5 +/- 0.1 nm [1].
References
[1]. gerhardt ma, wade sm, neubig rr. p-[125i]iodoclonidine is a partial agonist at the alpha 2-adrenergic receptor. mol pharmacol. 1990 aug;38(2):214-21.
